摘要:
A process is provided for the preparation of 10-deacetyl-N-debenzoyl-paclitaxel (I) a synthon useful for the preparation of taxanes with antitumour activity, and intermediates for the preparation thereof. Also described is a process for the preparation of Docetaxel starting from the compound of formula (I).
摘要:
Unsaturated esters of formula I ##STR1## in which R.sub.1, R.sub.2 and R.sub.3, which are the same or different to one another, represent hydrogen, hydroxyl, methoxyl or acetoxyl; n is between 13 and 25; are useful in the treatment of prostatic hyperplasia or hypertrophy.
摘要:
Compounds with a flavanone skeleton having the formula I ##STR1## in which R.sub.1 and R.sub.2, which may be the same or different, represent hydrogen, hydroxyl, methoxyl, thiomethyl, amino or substituted amino, are endowed with expectorant, mucolytic, mucopoietic, choleretic and hypolipaemia-producing activity.
摘要:
A soya extract having a content of glucoside isoflavones of at least 13% by weight and a content of 0.6 to 1.5 parts by weight of group B soya saponins per 1 part by weight of glucoside isoflavones. Also, pharmaceutical compositions containing this extract and methods of administering the extract to treat conditions such as pre- or post-menopausal symptoms, cancer, such as breast or prostrate cancer, or alcoholism. The extracts are made by a process which includes the steps of treating ripe whole soya beans or oil-free soya flour with an aliphatic alcohol to obtain a first extract; concentrating the first extract to form a concentrated first extract; purifying the concentrated first extract by treatment with at least one aliphatic hydrocarbon; and extracting active components from the purified concentrated first extract with a water-immiscible aliphatic alcohol to obtain a second extract. Preferably, the final extract is concentrated and dried to form the desired soya extract.
摘要:
The present invention relates to novel derivatives of 10-deacetylbaccatine III and of 10-deacetyl-14 .beta.-hydroxybaccatine III, having cytoxic and anti-tumoral activity. They are prepared starting from the so-called syntons or from other taxanes of natural origin, by selective oxidation of the hydroxyl in position 10 to keto function and subsequent esterification in position 13, if necessary, with isoserine chains variously substituted. The products of the invention can be administered by injection or orally, when suitably formulated.
摘要:
Isolation of a new taxane having pharmaceutical activity, 1a 14-beta-hydroxy-10-deacetyl-baccatine III and hemisynthesis of some derivatives useful as antitumor agents and intermediates.
摘要:
Isolation of a new taxane having pharmaceutical activity, 1a 14-beta-hydroxy-10-deacetyl-baccatine III and hemisynthesis of some derivatives useful as antitumor agents and intermediates.
摘要:
The preparation of new 3,11-cyclotaxanes having the general formula 1. Cyclotaxane 1a (1, R'.dbd.R".dbd.H) may be isolated from plants of the genus Taxus. New cyclotaxanes 1 have antiblastic activity.
摘要:
A process for the preparation of 10-deacetyl-bis-7,10-trichloroacetylbaccatin III (VI) said process comprising: reacting 10-deacetylbaccatin III with a trichloroacetic acid activated derivative to obtain a reaction mixture, and performing an isolation step on said reaction mixture obtain purified 10-deacetyl-bis-7,10-trichloroacetylbaccatin III (VI) having a content, of corresponding 7- or 10 mono-trichloroacetyl derivatives lower than 0.1% as determined by HPLC.
摘要:
A process is provided for the preparation of 10-deacetyl-N-debenzoyl-paclitaxel (I) a synthon useful for the preparation of taxanes with antitumour activity, and intermediates for the preparation thereof. Also described is a process for the preparation of Docetaxel starting from the compound of formula (I).